AU2003273855B2 - 2,7-substituted indoles and their use as 5-HT6 modulators - Google Patents

2,7-substituted indoles and their use as 5-HT6 modulators Download PDF

Info

Publication number: AU2003273855B2
Authority: AU; Australia
Prior art keywords: alkyl; indole; piperazin; benzenesulfonyl; optionally substituted
Prior art date: 2002-09-17
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Ceased

Application number

AU2003273855A

Other languages

English (en)

Other versions

AU2003273855A1 (en

Inventor

Ann Marie Madera

Robert James Weikert

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

F Hoffmann La Roche AG

Original Assignee

F Hoffmann La Roche AG

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2002-09-17

Filing date

2003-09-11

Publication date

2009-01-15

2003-09-11 Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG

2004-04-08 Publication of AU2003273855A1 publication Critical patent/AU2003273855A1/en

2009-01-15 Application granted granted Critical

2009-01-15 Publication of AU2003273855B2 publication Critical patent/AU2003273855B2/en

2023-09-11 Anticipated expiration legal-status Critical

Status Ceased legal-status Critical Current

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Neurology (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Psychiatry (AREA)
Psychology (AREA)
Hematology (AREA)
Child & Adolescent Psychology (AREA)
Diabetes (AREA)
Pain & Pain Management (AREA)
Obesity (AREA)
Hospice & Palliative Care (AREA)
Orthopedic Medicine & Surgery (AREA)
Physical Education & Sports Medicine (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Indole Compounds (AREA)
Plural Heterocyclic Compounds (AREA)

AU2003273855A 2002-09-17 2003-09-11 2,7-substituted indoles and their use as 5-HT6 modulators Ceased AU2003273855B2 (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US41123902P	2002-09-17	2002-09-17
US60/411,239		2002-09-17
PCT/EP2003/010101 WO2004026830A1 (en)	2002-09-17	2003-09-11	2,7-substituted indoles and their use as 5-ht6 modulators

Publications (2)

Publication Number	Publication Date
AU2003273855A1 AU2003273855A1 (en)	2004-04-08
AU2003273855B2 true AU2003273855B2 (en)	2009-01-15

Family

ID=32030655

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AU2003273855A Ceased AU2003273855B2 (en)	2002-09-17	2003-09-11	2,7-substituted indoles and their use as 5-HT6 modulators

Country Status (28)

Country	Link
US (1)	US7247651B2 (no)
EP (1)	EP1587788B9 (no)
JP (1)	JP4327091B2 (no)
KR (1)	KR100686758B1 (no)
CN (1)	CN1314669C (no)
AR (1)	AR041255A1 (no)
AT (1)	ATE362469T1 (no)
AU (1)	AU2003273855B2 (no)
BR (1)	BR0314352A (no)
CA (1)	CA2496765A1 (no)
DE (1)	DE60313895T2 (no)
DK (1)	DK1587788T3 (no)
ES (1)	ES2287518T3 (no)
GT (1)	GT200300199A (no)
HR (1)	HRP20050229A2 (no)
MX (1)	MXPA05002696A (no)
MY (1)	MY138826A (no)
NO (1)	NO20050666L (no)
NZ (1)	NZ537982A (no)
PA (1)	PA8582201A1 (no)
PE (1)	PE20050054A1 (no)
PL (1)	PL376020A1 (no)
PT (1)	PT1587788E (no)
RU (1)	RU2327685C2 (no)
TW (1)	TWI249402B (no)
UY (1)	UY27980A1 (no)
WO (1)	WO2004026830A1 (no)
ZA (1)	ZA200501306B (no)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US7452888B2 (en)	2002-03-27	2008-11-18	Glaxo Group Limited	Quinoline derivatives and their use as 5-ht6 ligands
BRPI0412263B1 (pt)	2003-07-22	2019-10-15	Arena Pharmaceuticals, Inc.	Derivados de diaril e aril heteroaril uréia, uso e composição farmacêutica contendo os mesmos, bem como processo para preparação da dita composição
PT1701940E (pt) *	2003-12-23	2008-07-30	Lundbeck & Co As H	Derivados de 2-(1h-indolilsulfanil)-benzil-amina como ssri
AR052308A1 (es) *	2004-07-16	2007-03-14	Lundbeck & Co As H	Derivados de 2-(1h-indolilsulfanil)-arilamina y una composicion farmaceutica que contiene al compuesto
CN102114244A (zh)	2004-09-30	2011-07-06	弗·哈夫曼-拉罗切有限公司	治疗认知障碍的组合物和方法
US7713954B2 (en) *	2004-09-30	2010-05-11	Roche Palo Alto Llc	Compositions and methods for treating cognitive disorders
WO2006062481A1 (en) *	2004-12-09	2006-06-15	Biovitrum Ab	New benzofuran derivatives and their use in the treatment of obesity, type ii diabetes and cns disorders .
US7629473B2 (en) *	2005-06-17	2009-12-08	H. Lundbeck A/S	2-(1H-indolylsulfanyl)-aryl amine derivatives
AR054393A1 (es) *	2005-06-17	2007-06-20	Lundbeck & Co As H	Derivados de benzo(b)furano y benzo(b)tiofeno, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de la reabsorcion de neurotransmisores de amina biogenicos.
CA2668959A1 (en) *	2006-11-09	2008-05-15	F. Hoffmann-La Roche Ag	Indole and benzofuran 2-carboxamide derivatives
EP2254564A1 (en)	2007-12-12	2010-12-01	Glaxo Group Limited	Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline
US20110021538A1 (en)	2008-04-02	2011-01-27	Arena Pharmaceuticals, Inc.	Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor
US9126946B2 (en)	2008-10-28	2015-09-08	Arena Pharmaceuticals, Inc.	Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto
CN103288707B (zh) *	2013-05-28	2015-12-23	浙江大学	一种3-苯巯基吲哚衍生物的制备方法
WO2015090233A1 (en)	2013-12-20	2015-06-25	Sunshine Lake Pharma Co., Ltd.	Aromatic heterocyclic compounds and their application in pharmaceuticals
CA2953004C (en)	2014-07-08	2023-02-21	Sunshine Lake Pharma Co., Ltd.	Aromatic heterocyclic derivatives and pharmaceutical applications thereof
WO2016201373A1 (en)	2015-06-12	2016-12-15	Axovant Sciences Ltd.	Diaryl and arylheteroaryl urea derivatives useful for the prophylaxis and treatment of rem sleep behavior disorder
CA2992518A1 (en)	2015-07-15	2017-01-19	Axovant Sciences Gmbh	Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of hallucinations associated with a neurodegenerative disease

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
FR2679903B1 (fr) *	1991-08-02	1993-12-03	Elf Sanofi	Derives de la n-sulfonyl indoline portant une fonction amidique, leur preparation, les compositions pharmaceutiques en contenant.
MX9700693A (es)	1994-07-26	1997-04-30	Pfizer	Derivados del 4-indol.
US6114532A (en) *	1998-02-03	2000-09-05	Boehringer Ingelheim Pharma Kg	Bicyclic heterocycles, the preparation thereof, and their use as pharmaceuticals
ATE225345T1 (de)	1998-06-30	2002-10-15	Lilly Co Eli	Auf serotonin-verwandte systeme wirkende piperidin-derivate
FR2788772B1 (fr) *	1999-01-26	2001-03-02	Adir	Nouveaux composes cyano-indoles inhibiteurs de recapture de serotonine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
GB9912413D0 (en)	1999-05-28	1999-07-28	Pfizer Ltd	Compounds useful in therapy
DE60122767T2 (de) *	2000-11-24	2007-09-13	Smithkline Beecham P.L.C., Brentford	Indoly-lsulphonyl-verbindungen zur behandlung von störungen des zns
MXPA03011244A (es) *	2001-06-07	2004-02-27	Hoffmann La Roche	Nuevos derivados de indol con afinidad por el receptor 5-ht6.
CA2450245A1 (en) *	2001-06-15	2002-12-27	F. Hoffmann-La Roche Ag	4-piperazinylindole derivatives with 5-ht6 receptor affinity
EP1414442A1 (en) *	2001-08-07	2004-05-06	Smithkline Beecham Plc	3-arylsulfonyl-7-piperazinyl- indoles, -benzofurans and -benzothiophenes with 5-ht6 receptor affinity for treating cns disorders
US7943639B2 (en)	2002-06-20	2011-05-17	Proximagen Limited	Compounds

2003
- 2003-09-11 EP EP03757820A patent/EP1587788B9/en not_active Expired - Lifetime
- 2003-09-11 AU AU2003273855A patent/AU2003273855B2/en not_active Ceased
- 2003-09-11 BR BR0314352-0A patent/BR0314352A/pt not_active IP Right Cessation
- 2003-09-11 PL PL03376020A patent/PL376020A1/xx not_active Application Discontinuation
- 2003-09-11 KR KR1020057004480A patent/KR100686758B1/ko not_active Expired - Fee Related
- 2003-09-11 CN CNB03821590XA patent/CN1314669C/zh not_active Expired - Fee Related
- 2003-09-11 NZ NZ537982A patent/NZ537982A/en unknown
- 2003-09-11 ES ES03757820T patent/ES2287518T3/es not_active Expired - Lifetime
- 2003-09-11 MX MXPA05002696A patent/MXPA05002696A/es active IP Right Grant
- 2003-09-11 PT PT03757820T patent/PT1587788E/pt unknown
- 2003-09-11 AT AT03757820T patent/ATE362469T1/de not_active IP Right Cessation
- 2003-09-11 CA CA002496765A patent/CA2496765A1/en not_active Abandoned
- 2003-09-11 DE DE60313895T patent/DE60313895T2/de not_active Expired - Lifetime
- 2003-09-11 RU RU2005111587/04A patent/RU2327685C2/ru not_active IP Right Cessation
- 2003-09-11 HR HR20050229A patent/HRP20050229A2/hr not_active Application Discontinuation
- 2003-09-11 DK DK03757820T patent/DK1587788T3/da active
- 2003-09-11 JP JP2004537044A patent/JP4327091B2/ja not_active Expired - Fee Related
- 2003-09-11 WO PCT/EP2003/010101 patent/WO2004026830A1/en not_active Ceased
- 2003-09-12 TW TW092125197A patent/TWI249402B/zh not_active IP Right Cessation
- 2003-09-12 PA PA20038582201A patent/PA8582201A1/es unknown
- 2003-09-12 PE PE2003000929A patent/PE20050054A1/es not_active Application Discontinuation
- 2003-09-15 AR ARP030103331A patent/AR041255A1/es unknown
- 2003-09-15 UY UY27980A patent/UY27980A1/es not_active Application Discontinuation
- 2003-09-16 MY MYPI20033528A patent/MY138826A/en unknown
- 2003-09-16 US US10/663,314 patent/US7247651B2/en not_active Expired - Fee Related
- 2003-09-16 GT GT200300199A patent/GT200300199A/es unknown
2005
- 2005-02-08 NO NO20050666A patent/NO20050666L/no not_active Application Discontinuation
- 2005-02-14 ZA ZA200501306A patent/ZA200501306B/xx unknown

Also Published As

Publication number	Publication date
CA2496765A1 (en)	2004-04-01
AU2003273855A1 (en)	2004-04-08
AR041255A1 (es)	2005-05-11
DE60313895D1 (de)	2007-06-28
DE60313895T2 (de)	2008-01-17
DK1587788T3 (da)	2007-09-24
GT200300199A (es)	2006-08-22
TW200410685A (en)	2004-07-01
ATE362469T1 (de)	2007-06-15
EP1587788A1 (en)	2005-10-26
ES2287518T3 (es)	2007-12-16
RU2005111587A (ru)	2005-11-20
PT1587788E (pt)	2007-08-20
PE20050054A1 (es)	2005-02-18
CN1681782A (zh)	2005-10-12
US20040063724A1 (en)	2004-04-01
PA8582201A1 (es)	2004-04-23
HK1083500A1 (en)	2006-07-07
CN1314669C (zh)	2007-05-09
PL376020A1 (en)	2005-12-12
KR100686758B1 (ko)	2007-02-26
BR0314352A (pt)	2005-07-19
WO2004026830A1 (en)	2004-04-01
NZ537982A (en)	2007-05-31
MY138826A (en)	2009-07-31
JP4327091B2 (ja)	2009-09-09
KR20050057357A (ko)	2005-06-16
EP1587788B1 (en)	2007-05-16
MXPA05002696A (es)	2005-05-05
EP1587788B9 (en)	2007-10-24
RU2327685C2 (ru)	2008-06-27
UY27980A1 (es)	2004-03-31
ZA200501306B (en)	2006-05-31
NO20050666L (no)	2005-03-11
US7247651B2 (en)	2007-07-24
TWI249402B (en)	2006-02-21
HRP20050229A2 (hr)	2006-04-30
JP2006503052A (ja)	2006-01-26

Publication	Publication Date	Title
AU2003273855B2 (en)	2009-01-15	2,7-substituted indoles and their use as 5-HT6 modulators
AU2003267063B2 (en)	2009-08-06	2,4-substituted indoles and their use as 5-HT6 modulators
DE60309498T2 (de)	2007-08-30	4-piperazinylbenzolsulfonyl-indole mit 5-ht6 rezeptor-affinität
US20030229069A1 (en)	2003-12-11	1-Sulfonyl-4-aminoalkoxy indole derivatives and uses thereof
ZA200309258B (en)	2005-02-28	4-Piperazinylindole derivatives with 5-HT6 receptor affinity.

Legal Events

Date	Code	Title	Description
2009-05-14	FGA	Letters patent sealed or granted (standard patent)
2011-04-07	MK14	Patent ceased section 143(a) (annual fees not paid) or expired